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Three novel ¹⁸F-labeled 4-aminoquinazoline derivatives, N-(3-chloro-4-fluorophenyl)-6-(2-[¹⁸F]fluoroethoxy)-7-methoxyquinazolin-4-amine([¹⁸F]1), N-(3-ethynylphenyl)-6-(2-[¹⁸F]fluoroethoxy)-7-methoxyquinazolin-4-amine([¹⁸F]2), and N-(3-bromophenyl)-6-(2-[¹⁸F]fluoroethoxy)-7-methoxyquinazolin-4-amine([¹⁸F]3) were synthesized and radiolabeled by two-step reaction with overall radiochemical yield of 21–24% (without decay corrected). Then we carried out their biodistribution experiments in S180 tumor-bearing mice. Results showed that they had certain concentration accumulation in tumor and fast clearance from muscle and blood. It was encouraging that [¹⁸F]3 was competitive among three ¹⁸F-labeled 4-aminoquinazoline derivatives in some aspects such as tumor/muscle uptake ratio reaching 7.70 at 60min post-injection, tumor/blood uptake ratio reaching 6.61 at 120min post-injection. So we …